LF 16.0335, a novel potent and selective nonpeptide antagonist of the human bradykinin B_2 receptor

摘要

In the present paper, we describe the in vitro pharmacological properties of LF 16.0335(1-[[3-[2,4- dimethylquinolin-8-yl)oxymethyl]-2, 4-dichloro-phenyl]sulphonyl]-2(S)-[[4-[4-(aminoiminomethy)phenyl- carbonyl]piperazin-1-yl]carbonyl]pyrrolidine), a novel and potent nonpeptide antagonist of the human bradykinin (BK) B_2 receptor. LF 16.0335 displaced [~3H]-BK binding to membrane preparations from CHO cells expressing the Cloned human B_2 receptor, INT 407 cells and human umbilical vein with K_I values of 0.84±0.39 nM, 1.26±0.68 nM and 2.34±0.36 nM, respectively.